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In vivo studies of fullerene-based materials using endohedral metallofullerene radiotracers
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| Zeitschriftentitel: | Proceedings of the National Academy of Sciences |
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| Personen und Körperschaften: | , , , , |
| In: | Proceedings of the National Academy of Sciences, 96, 1999, 9, S. 5182-5187 |
| Format: | E-Article |
| Sprache: | Englisch |
| veröffentlicht: |
Proceedings of the National Academy of Sciences
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| Schlagwörter: |
| Zusammenfassung: | <jats:p> Biodistribution studies of a water-soluble radioactive metallofullerene compound have been conducted using BALB/c mice. To this end, a sample containing Ho <jats:sub>x</jats:sub> @C <jats:sub>82</jats:sub> (x = 1, 2) was purified and derivatized to prepare the water-soluble metallofullerol, Ho <jats:sub>x</jats:sub> @C <jats:sub>82</jats:sub> (OH) <jats:sub>y</jats:sub> . This metallofullerol was then neutron-activated ( <jats:sup>165</jats:sup> Ho[n,γ] <jats:sup>166</jats:sup> Ho) to prepare the <jats:sup>166</jats:sup> Ho <jats:sub>x</jats:sub> @C <jats:sub>82</jats:sub> (OH) <jats:sub>y</jats:sub> analog as a radiotracer, which was monitored, after intravenous administration, for up to 48 hours by using dissection radioanalysis, and its biodistribution was compared with a control compound, Na <jats:sub>2</jats:sub> [ <jats:sup>166</jats:sup> Ho(DTPA)(H <jats:sub>2</jats:sub> O)]. Results showed selective localization of the <jats:sup>166</jats:sup> Ho <jats:sub>x</jats:sub> @C <jats:sub>82</jats:sub> (OH) <jats:sub>y</jats:sub> tracer in the liver but with slow clearance, as well as uptake by bone without clearance. In contrast, excretion of the control compound was nearly quantitative after 1 hour. The fate of <jats:sup>166</jats:sup> Ho was also explored by a metabolism study of <jats:sup>166</jats:sup> Ho <jats:sub>x</jats:sub> @C <jats:sub>82</jats:sub> (OH) <jats:sub>y</jats:sub> in Fischer rats. Results indicated 20% excretion of intact <jats:sup>166</jats:sup> Ho <jats:sub>x</jats:sub> @C <jats:sub>82</jats:sub> (OH) <jats:sub>y</jats:sub> within 5 days. The present findings demonstrate the feasibility of using water-solubilized metallofullerene radiotracers to monitor the fate of fullerene-based materials in animals, and suggest that water-solubilized fullerene materials, in general, may be useful components in drug design. </jats:p> |
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| Umfang: | 5182-5187 |
| ISSN: |
0027-8424
1091-6490 |
| DOI: | 10.1073/pnas.96.9.5182 |